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FEBS Lett. 2009 Jul 7;583(13):2208-12. doi: 10.1016/j.febslet.2009.06.017. Epub 2009 Jun 13.

A selective small-molecule inhibitor of c-Jun N-terminal kinase 1.

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1
The Hormel Institute, University of Minnesota, Austin, MN 55912, USA.

Abstract

Indiscriminately suppressing total c-Jun N-terminal kinase (JNK) activity is not an appropriate strategy because each JNK appears to have a distinct function in cancer, asthma, diabetes, or Parkinson's disease. Herein, we report that 7-(6-N-phenylaminohexyl)amino-2H-anthra[1,9-cd]pyrazol-6-one (AV-7) inhibited JNK1 activity, but not JNK2 or JNK3. We found that ultraviolet B (UVB) induced c-Jun phosphorylation and sub-G1 accumulation in JNK2(-/-) murine embryonic fibroblasts, which contain an abundance of JNK1, but not JNK2. These results demonstrate that AV-7 is an isoform selective small-molecule inhibitor of JNK1 activity, which might be developed as a therapeutic against diabetes.

PMID:
19527717
DOI:
10.1016/j.febslet.2009.06.017
[Indexed for MEDLINE]
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